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RU2013149635A - SOLIFENACIN COMPOUNDS AND SALIVARY STIMULANTS FOR THE TREATMENT OF URINE BUBBLE HYPERACTIVITY - Google Patents

SOLIFENACIN COMPOUNDS AND SALIVARY STIMULANTS FOR THE TREATMENT OF URINE BUBBLE HYPERACTIVITY Download PDF

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RU2013149635A
RU2013149635A RU2013149635/15A RU2013149635A RU2013149635A RU 2013149635 A RU2013149635 A RU 2013149635A RU 2013149635/15 A RU2013149635/15 A RU 2013149635/15A RU 2013149635 A RU2013149635 A RU 2013149635A RU 2013149635 A RU2013149635 A RU 2013149635A
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pharmaceutically acceptable
acceptable salt
solifenacin
pilocarpine
present
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Мехди ПАБОРДЖИ
Венди Джейд Лимайо ЭРНАНДЕС
Кеннет Л. ДАЧИН
Роджер С. ФЛЮГЕЛ
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Теравида, Инк.
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Urology & Nephrology (AREA)
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Abstract

1. Фармацевтическая композиция, включающая терапевтически эффективное количество солифенацина пролонгированного действия или его фармацевтически приемлемой соли и терапевтически эффективное количество пилокарпина или его фармацевтически приемлемой соли.2. Композиция по п.1, отличающаяся тем, что солифенацин или его фармацевтически приемлемая соль и пилокарпин или его фармацевтически приемлемая соль находятся совместно в одной и той же лекарственной форме.3. Композиция по п.1, отличающаяся тем, что солифенацин или его фармацевтически приемлемая соль присутствует в дозе от 0,1 мг до 50 мг.4. Композиция по п.1, отличающаяся тем, что солифенацин или его фармацевтически приемлемая соль присутствует в дозе, выбранной из группы, состоящей из 1 мг, 2 мг, 3 мг, 4 мг, 5 мг, 6 мг, 7 мг, 8 мг, 10 мг, 12 мг, 14 мг, 16 мг или 20 мг.5. Композиция по п.1, отличающаяся тем, что пилокарпин или его фармацевтически приемлемая соль присутствует в дозе от 0,1 мг до 50 мг.6. Композиция по п.1, отличающаяся тем, что пилокарпин или его фармацевтически приемлемая соль присутствует в дозе, выбранной из группы, состоящей из 1 мг, 2 мг, 3 мг, 4 мг или 4,5 мг, 5 мг, 5,5 мг, 6 мг, 6,5 мг, 7 мг, 7,5 мг, 8 мг, 8,5 мг, 9 мг, 9,5 мг, 10 мг, 10,5 мг, 11 мг, 11,5 мг, 12 мг, 13 мг и 15 мг.7. Композиция по п.1, отличающаяся тем, что дополнительно включает фармацевтически приемлемый носитель, разбавитель или наполнитель.8. Способ лечения пациента, страдающего от гиперактивного мочевого пузыря, включающий:идентификацию пациента, нуждающегося в этом, ивведение пациенту терапевтически эффективного количества солифенацина пролонгированного действия или его фармацевтически приемлемой соли и терапевтически эффективного кол1. A pharmaceutical composition comprising a therapeutically effective amount of sustained-release solifenacin or a pharmaceutically acceptable salt thereof and a therapeutically effective amount of pilocarpine or a pharmaceutically acceptable salt thereof. The composition according to claim 1, characterized in that solifenacin or its pharmaceutically acceptable salt and pilocarpine or its pharmaceutically acceptable salt are together in the same dosage form. The composition according to claim 1, characterized in that solifenacin or a pharmaceutically acceptable salt thereof is present in a dose of from 0.1 mg to 50 mg. The composition according to claim 1, characterized in that solifenacin or a pharmaceutically acceptable salt thereof is present in a dose selected from the group consisting of 1 mg, 2 mg, 3 mg, 4 mg, 5 mg, 6 mg, 7 mg, 8 mg, 10 mg, 12 mg, 14 mg, 16 mg or 20 mg. 5. The composition according to claim 1, characterized in that pilocarpine or its pharmaceutically acceptable salt is present in a dose of from 0.1 mg to 50 mg. The composition according to claim 1, characterized in that pilocarpine or its pharmaceutically acceptable salt is present in a dose selected from the group consisting of 1 mg, 2 mg, 3 mg, 4 mg or 4.5 mg, 5 mg, 5.5 mg 6 mg, 6.5 mg, 7 mg, 7.5 mg, 8 mg, 8.5 mg, 9 mg, 9.5 mg, 10 mg, 10.5 mg, 11 mg, 11.5 mg, 12 mg, 13 mg and 15 mg. 7. A composition according to claim 1, characterized in that it further comprises a pharmaceutically acceptable carrier, diluent or excipient. A method for treating a patient suffering from an overactive bladder, comprising: identifying a patient in need thereof and administering to the patient a therapeutically effective amount of sustained-release solifenacin or a pharmaceutically acceptable salt thereof and a therapeutically effective number

Claims (20)

1. Фармацевтическая композиция, включающая терапевтически эффективное количество солифенацина пролонгированного действия или его фармацевтически приемлемой соли и терапевтически эффективное количество пилокарпина или его фармацевтически приемлемой соли.1. A pharmaceutical composition comprising a therapeutically effective amount of sustained-release solifenacin or a pharmaceutically acceptable salt thereof and a therapeutically effective amount of pilocarpine or a pharmaceutically acceptable salt thereof. 2. Композиция по п.1, отличающаяся тем, что солифенацин или его фармацевтически приемлемая соль и пилокарпин или его фармацевтически приемлемая соль находятся совместно в одной и той же лекарственной форме.2. The composition according to claim 1, characterized in that solifenacin or its pharmaceutically acceptable salt and pilocarpine or its pharmaceutically acceptable salt are together in the same dosage form. 3. Композиция по п.1, отличающаяся тем, что солифенацин или его фармацевтически приемлемая соль присутствует в дозе от 0,1 мг до 50 мг.3. The composition according to claim 1, characterized in that solifenacin or its pharmaceutically acceptable salt is present in a dose of from 0.1 mg to 50 mg. 4. Композиция по п.1, отличающаяся тем, что солифенацин или его фармацевтически приемлемая соль присутствует в дозе, выбранной из группы, состоящей из 1 мг, 2 мг, 3 мг, 4 мг, 5 мг, 6 мг, 7 мг, 8 мг, 10 мг, 12 мг, 14 мг, 16 мг или 20 мг.4. The composition according to claim 1, characterized in that solifenacin or its pharmaceutically acceptable salt is present in a dose selected from the group consisting of 1 mg, 2 mg, 3 mg, 4 mg, 5 mg, 6 mg, 7 mg, 8 mg, 10 mg, 12 mg, 14 mg, 16 mg or 20 mg. 5. Композиция по п.1, отличающаяся тем, что пилокарпин или его фармацевтически приемлемая соль присутствует в дозе от 0,1 мг до 50 мг.5. The composition according to claim 1, characterized in that pilocarpine or its pharmaceutically acceptable salt is present in a dose of from 0.1 mg to 50 mg. 6. Композиция по п.1, отличающаяся тем, что пилокарпин или его фармацевтически приемлемая соль присутствует в дозе, выбранной из группы, состоящей из 1 мг, 2 мг, 3 мг, 4 мг или 4,5 мг, 5 мг, 5,5 мг, 6 мг, 6,5 мг, 7 мг, 7,5 мг, 8 мг, 8,5 мг, 9 мг, 9,5 мг, 10 мг, 10,5 мг, 11 мг, 11,5 мг, 12 мг, 13 мг и 15 мг.6. The composition according to claim 1, characterized in that pilocarpine or its pharmaceutically acceptable salt is present in a dose selected from the group consisting of 1 mg, 2 mg, 3 mg, 4 mg or 4.5 mg, 5 mg, 5, 5 mg, 6 mg, 6.5 mg, 7 mg, 7.5 mg, 8 mg, 8.5 mg, 9 mg, 9.5 mg, 10 mg, 10.5 mg, 11 mg, 11.5 mg , 12 mg, 13 mg and 15 mg. 7. Композиция по п.1, отличающаяся тем, что дополнительно включает фармацевтически приемлемый носитель, разбавитель или наполнитель.7. The composition according to claim 1, characterized in that it further comprises a pharmaceutically acceptable carrier, diluent or excipient. 8. Способ лечения пациента, страдающего от гиперактивного мочевого пузыря, включающий:8. A method of treating a patient suffering from an overactive bladder, comprising: идентификацию пациента, нуждающегося в этом, иidentification of the patient in need of it, and введение пациенту терапевтически эффективного количества солифенацина пролонгированного действия или его фармацевтически приемлемой соли и терапевтически эффективного количества пилокарпина или его фармацевтически приемлемой соли.administering to the patient a therapeutically effective amount of sustained-release solifenacin or a pharmaceutically acceptable salt thereof and a therapeutically effective amount of pilocarpine or a pharmaceutically acceptable salt thereof. 9. Способ по п.8, отличающийся тем, что солифенацин или его фармацевтически приемлемая соль, и пилокарпин или его фармацевтически приемлемая соль находятся совместно в одной и той же лекарственной форме.9. The method according to claim 8, characterized in that solifenacin or its pharmaceutically acceptable salt, and pilocarpine or its pharmaceutically acceptable salt are together in the same dosage form. 10. Способ по п.8, отличающийся тем, что солифенацин или его фармацевтически приемлемую соль и пилокарпин или его фармацевтически приемлемую соль вводят раздельно.10. The method according to claim 8, characterized in that solifenacin or its pharmaceutically acceptable salt and pilocarpine or its pharmaceutically acceptable salt are administered separately. 11. Способ по п.8, отличающийся тем, что солифенацин или его фармацевтически приемлемая соль присутствует в дозе от 0,1 мг до 50 мг.11. The method according to claim 8, characterized in that solifenacin or its pharmaceutically acceptable salt is present in a dose of from 0.1 mg to 50 mg. 12. Способ по п.8, отличающийся тем, что солифенацин или его фармацевтически приемлемая соль присутствует в дозе, выбранной из группы, состоящей из 1 мг, 2 мг, 3 мг, 4 мг, 5 мг, 6 мг, 7 мг, 8 мг, 10 мг, 12 мг, 14 мг, 15 мг, 16 мг или 20 мг.12. The method according to claim 8, characterized in that solifenacin or a pharmaceutically acceptable salt thereof is present in a dose selected from the group consisting of 1 mg, 2 mg, 3 mg, 4 mg, 5 mg, 6 mg, 7 mg, 8 mg, 10 mg, 12 mg, 14 mg, 15 mg, 16 mg or 20 mg. 13. Способ по п.8, отличающийся тем, что пилокарпин или его фармацевтически приемлемая соль присутствует в дозе от 0,1 мг до 50 мг.13. The method according to claim 8, characterized in that pilocarpine or its pharmaceutically acceptable salt is present in a dose of from 0.1 mg to 50 mg. 14. Способ по п.8, отличающийся тем, что пилокарпин или его фармацевтически приемлемая соль присутствует в дозе, выбранной из группы, состоящей из 1 мг, 2 мг, 3 мг, 4 мг или 4,5 мг, 5 мг, 5,5 мг, 6 мг, 6,5 мг, 7 мг, 7,5 мг, 8 мг, 8,5 мг, 9 мг, 9,5 мг, 10 мг, 10,5 мг, 11 мг, 11,5 мг, 12 мг, 13 мг и 15 мг.14. The method according to claim 8, characterized in that pilocarpine or its pharmaceutically acceptable salt is present in a dose selected from the group consisting of 1 mg, 2 mg, 3 mg, 4 mg or 4.5 mg, 5 mg, 5, 5 mg, 6 mg, 6.5 mg, 7 mg, 7.5 mg, 8 mg, 8.5 mg, 9 mg, 9.5 mg, 10 mg, 10.5 mg, 11 mg, 11.5 mg , 12 mg, 13 mg and 15 mg. 15. Способ облегчения побочных эффектов лечения гиперактивного мочевого пузыря у пациента, страдающего от этого заболевания, включающий:15. A method of alleviating the side effects of treating an overactive bladder in a patient suffering from this disease, comprising: идентификацию пациента, нуждающегося в этом, иidentification of the patient in need of it, and введение пациенту терапевтически эффективного количества солифенацина пролонгированного действия или его фармацевтически приемлемой соли и терапевтически эффективного количества пилокарпина или его фармацевтически приемлемой соли.administering to the patient a therapeutically effective amount of sustained-release solifenacin or a pharmaceutically acceptable salt thereof and a therapeutically effective amount of pilocarpine or a pharmaceutically acceptable salt thereof. 16. Способ по п.15, отличающийся тем, что солифенацин или его фармацевтически приемлемая соль и пилокарпин или его фармацевтически приемлемая соль, находятся совместно в одной и той же лекарственной форме.16. The method according to clause 15, wherein the solifenacin or its pharmaceutically acceptable salt and pilocarpine or its pharmaceutically acceptable salt are together in the same dosage form. 17. Способ по п.15, отличающийся тем, что солифенацин или его фармацевтически приемлемая соль присутствует в дозе от 0,1 мг до 50 мг.17. The method according to clause 15, wherein the solifenacin or its pharmaceutically acceptable salt is present in a dose of from 0.1 mg to 50 mg. 18. Способ по п.15, отличающийся тем, что солифенацин или его фармацевтически приемлемая соль присутствует в дозе, выбранной из группы, состоящей из 1 мг, 2 мг, 3 мг, 4 мг, 5 мг, 6 мг, 7 мг, 8 мг, 10 мг, 12 мг, 14 мг, 15 мг, 16 мг или 20 мг.18. The method according to clause 15, wherein the solifenacin or its pharmaceutically acceptable salt is present in a dose selected from the group consisting of 1 mg, 2 mg, 3 mg, 4 mg, 5 mg, 6 mg, 7 mg, 8 mg, 10 mg, 12 mg, 14 mg, 15 mg, 16 mg or 20 mg. 19. Способ по п.15, отличающийся тем, что пилокарпин или его фармацевтически приемлемая соль присутствует в дозе от 0,1 мг до 50 мг.19. The method according to clause 15, wherein the pilocarpine or its pharmaceutically acceptable salt is present in a dose of from 0.1 mg to 50 mg. 20. Способ по п.15, отличающийся тем, что пилокарпин или его фармацевтически приемлемая соль присутствует в дозе, выбранной из группы, состоящей из 1 мг, 2 мг, 3 мг, 4 мг или 4,5 мг, 5 мг, 5,5 мг, 6 мг, 6,5 мг, 7 мг, 7,5 мг, 8 мг, 8,5 мг, 9 мг, 9,5 мг, 10 мг, 10,5 мг, 11 мг, 11,5 мг, 12 мг, 13 мг и 15 мг. 20. The method according to clause 15, wherein the pilocarpine or its pharmaceutically acceptable salt is present in a dose selected from the group consisting of 1 mg, 2 mg, 3 mg, 4 mg or 4.5 mg, 5 mg, 5, 5 mg, 6 mg, 6.5 mg, 7 mg, 7.5 mg, 8 mg, 8.5 mg, 9 mg, 9.5 mg, 10 mg, 10.5 mg, 11 mg, 11.5 mg , 12 mg, 13 mg and 15 mg.
RU2013149635A 2011-05-10 2012-05-09 Appliance of solifenacin and saliva flow stimulators for the treatment of overactive bladder RU2671575C2 (en)

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